B / 31 : Drugs Used In Cancer Treatment III (Topoisomerase And Mitotic Spindle Inhibitors) Flashcards
1
Q
What is topoisomerase I?
A
Enzyme which cuts one of the two strands of dsDNA
2
Q
What is topoisomerase II?
A
Enzyme which cuts both strands of dsDNA to unwind DNA
3
Q
What are 3 topoisomerase inhibitors?
A
- Doxorubicin
- Irinotecan
- Etoposide
4
Q
Irinotecan
- MOA
- Effect
- Indication
- SE
A
- Topoisomerase I inhibitor
- Inhibition of transcription + replication
- For colon cancer
- BM suppression, GI disturbances
5
Q
Etoposide, Doxorubicin
- MOA
- Effect
- Indication
- SE
A
- Topoisomerase II inhibitor
- dsDNA breaks : apoptosis induction
- For Hodgkin and non Hodgkin lymphomas, leukemia, breast cancer, lung cancer
- Usual + cardiotoxicity (doxorubicin)
(Edgar Allan POE + TOPhat + ruby for doxoRUBYcin)
6
Q
How do inhibitors of mitotic spindle act?
A
They affect the equilibrium between polymerized and depolymerized forms of the microtubules
7
Q
What are the mitotic spindle inhibitor drugs?
A
- Vincristine
- Docetaxel
8
Q
Vincristine
- MOA
- Effect
- Indication
- SE
A
- Inhibits microtubule polymerization : disruption of assembly of microtubules
- Inhibition of cell division and mitosis
- For Leukemia, Hodgkin and non Hodgkin lymphomas, solid tumors
- Usual + neurotoxicity
9
Q
Docetaxel
- MOA
- Effect
- Indication
- SE
A
- Inhibits microtubule depolymerization : inhibits disassembly into monomers
- Inhibition of cell division + mitosis
- Breast, ovarian, lung cancers
- BM suppression, cardiotoxicity, neurotoxicity
10
Q
When do inhibitors of mitotic spindle act?
A
CCS : during M phase
11
Q
When do topoisomerase inhibitors act?
A
CCS : S phase, except doxorubicin which is CCNS
